5-Fluorouracil Derivatives. XII. : Synthesis and Antitumor Activity of α-Alkylthiomethyl-, α-Alkylsulfinylmethyl-, α-Alkylsulfonylmethyl-, and α-Acylthiomethyl-5-fluorouracils(Medeicinal Chemistry,Chemical)

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概要

• 論文の詳細を見る

• For the purpose of diminishing the toxicity of 5-fluorouracil (1) and obtaining biologically active derivatives of 1 suitable for oral administration, alkylthiomethyl, alkylsulfinylmethyl, alkylsulfonylmethyl, and acylthiomethyl groups were introduced at the 1- and 3-positions of 1. The antitumor activity of these synthetic compounds was tested against L1210 leukemia in mice. 1-Alkylthiomethyl-5-fluorouracils showed weak antitumor activity at a high dose (300 mg/kg).

• 社団法人日本薬学会の論文
• 1987-09-25

著者

• Hoshi Akio

  国立がんセンター

• Hoshi Akio

  National Cancer Center Research Institute

• MORI HARUKI

  Research Center, Mitsui Toatsu Chemicals

• IIGO MASAAKI

  National Cancer Center Research Institute

• Hoshi A

  National Cancer Center Resarch Institute

• Iigo Masaaki

  National Cancer Center Resarch Institute

• OZAKI SHOICHIRO

  Faculty of Engineering, Ehime University

• NAGASE TOSHIO

  Faculty of Engineering, Ehime University

• TAMAI HIROFUMI

  Faculty of Engineering, Ehime University

• Mori H

  Kumamoto Univ. Kumamoto Jpn

• Ozaki S

  Faculty Of Pharmaceutical Sciences Osaka University

• Nagase T

  Faculty Of Engineering Ehime University

• Tamai Hirofumi

  Faculty Of Engineering Ehime University

• HOSHI Akio

  National Cancer Center Resarch Institute

関連論文

• 5-Fluorouracil Derivatives. X. : Synthesis and Antitumor Activities of α-Alkoxyalkyl-5-fluorouracils
• 5-Fluorouracil Derivatives. XXII. Synthesis and Antitumor Activities of 1-Carbamoyl-5-fluorouracils
• 5-Fluorouracil Derivatives. XII. : Synthesis and Antitumor Activity of α-Alkylthiomethyl-, α-Alkylsulfinylmethyl-, α-Alkylsulfonylmethyl-, and α-Acylthiomethyl-5-fluorouracils(Medeicinal Chemistry,Chemical)
• Retention of CPT-11 in the Pancreas and Liver Following Daily Administration to Athymic Mice
• ANTITUMOR ACTIVITY OF 1-ACYLOXYMETHYL DERIVATIVES OF 5-FLUOROURACIL AGAINST L1210 LEUKEMIA
• ANTITUMOR ACTIVITY OF ALKYLDISULFIDE DERIVATIVES OF 6-MERCAPTOPURINES AGAINST L-1210 LEUKEMIA
• ANTITUMOR ACTIVITY OF 1-ALKOXYCARBONYLALKYLCAR-BAMOYL-5-FLUOROURACIL DERIVATIVES BY ORAL ADMINISTRATION
• STRUCTURE-ANTITUMOR ACTIVITY RELATIONSHIP OF PURIN-6-YL ALKYL DISULFIDES
• SYNTHETIC NUCLEOSIDES AND NUCLEOTIDES. X. SYNTHESIS AND BIOLOGICAL ACTIVITIES OF SEVERAL PURIN-6-YL BENZYL DISULFIDES AND THEIR RIBONUCLEOSIDES
• ANTITUMOR ACTIVITY OF DERIVATIVES OF NEPLANOCIN A IN VIVO AND IN VITRO
• ISOLATION AND CHARACTERIZATION OF THE MURINE LYMPHOMA L5178Y CELL LINE HIGHLY RESISTANT TO 5-FLUOROURACIL
• THE DIFFERENCE IN MECHANISM OF ACTION OF 5-FLUOROURACIL AND ITS NUCLEOSIDES IN L5178Y CELLS
• BIOLOGICAL ACTIVITY OF VITAMIN D_3 DERIVATIVES IN INDUCING DIFFERENTIATION OF HL-60 HUMAN PROMYELOCYTIC LEUKEMIA CELLS
• IMPROVEMENT OF THERAPEUTIC EFFECT OF 5-FLUOROURACIL BY OROTIC ACID
• EFFECT OF PYRIMIDINES, PURINES AND THEIR NUCLEOSIDES ON ANTITUMOR ACTIVITY OF 5-FLUOROURACIL AGAINST L-1210 LEUKEMIA
• EXCRETION OF 1-HEXYLCARBAMOYL-5-FLUOROURACIL IN URINE OF MICE
• ANTITUMOR ACTIVITY OF METABOLITES OF 1-HEXYLCAR-BAMOYL-5-FLUOROURACIL AND RELATED COMPOUNDS AGAINST L1210 LEUKEMIA IN VIVO AND L5178Y LYMPHOMA CELLS IN VITRO
• RELATIONSHIP BETWEEN CHEMICAL STRUCTURE AND ANTITUMOR ACTIVITY OF WITHAFERIN A ANALOGUES
• DISTRIBUTION OF 1-HEXYLCARBAMOYL-5-FLUOROURACIL AND 5-FLUOROURACIL BY ORAL ADMINISTRATION IN MICE
• ANTITUMOR ACTIVITY OF 1-HEXYLCARBAMOYL-5-FLUOROURACIL IN LEWIS LUNG CARCINOMA AND B16 MELANOMA
• ANTITUMOR AGENTS IN NUCLEIC ACID ANALOGUES
• Stereoselective Construction of Tetrahydrofuran by Tin (IV) Chloride Promoted [3+2] Cycloaddition of Allylsilane to α-Keto Ester
• Diastereoselective Addition of Organometallics to α-Keto Esters Bearing chiro-Inositol Derivatives as Chiral Auxiliaries
• Stereoselective Radical Addition to α-Methylenebutyrolactones by Indirect Electroreduction Catalyzed by a Nickel(II) Complex
• PC57 SYNTHESIS OF INOSITOL POLYPHOSPHATES
• 5-Fluorouracil derivatives. I. The synthesis of 1-carbamoyl-5-fluorouracils.

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